Suicide Substrates/Mechanism-based Inhibitors - Medicinal Chemistry 1.14

Suicide inhibitors or mechanism-based inhibitors are a type of highly-specific irreversible inhibitors that targets and hijacks the normal enzymatic reaction mechanism to inactivate the enzymes. They are relatively unreactive in cells or solution until they bind to the enzyme active site. For most of the irreversible inhibitors, the reactive functional groups are already present when the molecules are before reaching the target enzymes, which can make the inhibitor indiscriminately reactive. Suicide inhibitors initially bind to the enzyme like substrates and start going through the normal catalytic process. But they cannot be turned into products and released, which causes enzyme inhibition.
Two examples would be clavulanic acid and tienilic acid.
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I am a computational chemist in the pharmaceutical industry. I created the Mole Man Chem channel to explain some basic medicinal and biochemistry concepts because I believe the best way to relearn a concept is through teaching.
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[@comfortable_east]

This was extremely helpful!
Thank you, good sir.

[@Sunnysir9]

Super informative!! Love the content man keep it up!

[@molemanchem4385]

Thanks a lot!

[@MrHutchacademy]

Awesome video man. Keep it up!

[@molemanchem4385]

Thanks! Will do!

[@jesseallaway1149]

Nice video! Hadn't heard of these.

[@molemanchem4385]

Glad you enjoyed it!

[@umyeenabashir1948]

Can you do a video on unstable irreversible inhibitors?

[@molemanchem4385]

Hi Umyeena, thanks for the comment. I assume you are referring to the chemical stability of the inhibitors. Some irreversible inhibitors have high intrinsic reactivity ("unstable") due to a highly reactive fragment (usually an electrophile), which could be a double edge sword. I plan to make a video on that when I talk about pharmacokinetics (i.e., whole blood stability and GSH stability). If you have specific questions, feel free to email me at [e-mail] :)